Journal of Medicinal Chemistry p. 214 - 217 (1983)
Update date:2022-08-04
Topics: Experimental Receptor cannabinoids antihypertensive clinical trial hypotension
Zaugg, Harold E.
Kyncl, Jaroslav
A number of azacannabinoids containing hydroxyacyl and aminoacetyl substituents on the nitrogen atom were synthesized.The hydroxyacetyl and γ-hydroxybutyryl derivatives (4a and 7b, respectively) were potent antihypertensive agents (minimum effective dose, 3-5 mg/kg, orally) of the same order of activity as the highly CNS-active N-propargyl derivatives Ia and Ib.Furthermore, 4a showed weak stimulant properties at hypotensive dose levels, in contrast to the strongly CNS-depressant action characteristic of the N-propargyl analogues (Ia,b).
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(1982)